Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

2-D08 (2’,3’,4’-trihydroxyflavone) is a Sumoylation inhibitor.

Protein sumoylation is a dynamic posttranslational modification involved in various biological processes, such as cellular homeostasis and development. Sumoylation has been reported to play a key role in cancer, though so far there are few small molecule probes available.

In vitro: 2-D08 was identified as a cell permeable, mechanistically unique inhibitor of protein sumoylation. This compound was found to be able to block sumoylation of topoisomerase I in two different cancer cell lines when co-dosed with camptothecin. In addition, futher analyses indicated that 2-D08 inhibited sumoylation via preventing transfer of small ubiquitin-like modifier (SUMO) from the UBC9-SUMO thioester to the substrate without affecting SUMO-activating enzyme E1 (SAE-1/2) or E2 Ubc9-SUMO thioester formation, a mechanism of action that was unprecedented before [1]. Moreover, it was found that 2-D08 at 100 μM could effectively inhibit 10 μM Camptothecin induced Topoisomerase I SUMOylation in breast cancer without affecting overall cellular protein ubiquitinations [2].

In vivo: Up to now, there is no animal in vivo data reported for 2-D08.